Patents Assigned to Merck, Sharp & Dohms, Corp.
  • Automatic protein crystallization trial analysis system
    Patent number: 11010591
    Abstract: A protein crystallization trial is automatically analyzed by capturing images of the protein drops in the trial. A machine-learned model, such as a neural network, is applied to classify the images. The model generates a predicted classification from among a set of possible classifications which includes one or more crystal type classifications and one or more non-crystal type classifications. Users may be notified automatically of newly identified crystals (e.g., drops that are classified as a crystal type). The notification may include a link to a user interface that includes results of the trial.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: May 18, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Soheil Ghafurian, Ilknur Icke, Charles A. Lesburg, Belma Dogdas
  • Combinations of PD-1 Antagonists and Benzo[b]thiophene STING Agonists for Cancer Treatment
    Publication number: 20210130466
    Abstract: Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one benzo[b]thiophene compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.
    Type: Application
    Filed: July 30, 2018
    Publication date: May 6, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Saso CEMERSKI, Jared N. CUMMING, Johnny E. KOPINJA, Samanthi A. PERERA, Benjamin Wesley TROTTER, Archie Ngai-Chiu TSE
  • Substituted biaryl compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
    Patent number: 10995085
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: March 16, 2020
    Date of Patent: May 4, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yongxin Han, Abdelghani Achab, Yongqi Deng, Xavier Fradera, Craig Gibeau, Brett A. Hopkins, Derun Li, Kun Liu, Meredeth A. McGowan, Nunzio Sciammetta, David Sloman, Catherine White, Hongjun Zhang, Hua Zhou
  • Modulation of tumor immunity
    Patent number: 10994008
    Abstract: Methods of treating proliferative disorders are described. In particular, combination treatment with a GITR agonist and a PD-1 antagonist are provided.
    Type: Grant
    Filed: March 20, 2018
    Date of Patent: May 4, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gu Danling, Amy M. Beebe
  • NOVEL PROCESS FOR SYNTHESIS OF A PHENOXY DIAMINOPYRIMIDINE COMPOUND
    Publication number: 20210122717
    Abstract: Disclosed herein is a novel process for preparing Compound A free base, 5-((2,4-diaminopyrimidin-5-yl)oxy)-4-iso-propyl-2-methoxybenzenesulfonamide, and a citrate salt of Compound A with simplified chemistry and a high overall yield: Compound A. In one embodiment, the overall yield from the starting material 2-isopropylphenol to Compound A citrate salt is greater than 50%. In another embodiment, the overall yield is greater than 60%. Also disclosed herein are novel salts and solvates of Compound A.
    Type: Application
    Filed: April 18, 2019
    Publication date: April 29, 2021
    Applicants: Merck Sharp & Dohme Corp., Werthenstein BioPharma GmbH
    Inventors: Kevin M. Maloney, Kallol Basu, John Y.L. Chung, Richard Desmond, Michael James Di Maso, Guy R. Humphrey, Alfred Y. Lee, Dan Lehnherr, Feng Peng, Hong Ren, Mark Weisel, Siwei Zhang, Patrick Larpent
  • BIOMARKERS FOR A COMBINATION THERAPY COMPRISING LENVATINIB AND A PD-1 ANTAGONIST
    Publication number: 20210123919
    Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a combination therapy comprising lenvatinib compound and a PD-1 antagonist. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having, suspected of having, or at risk of developing cancer.
    Type: Application
    Filed: May 13, 2019
    Publication date: April 29, 2021
    Applicants: Merck Sharp & Dohme Corp., Eisai R&D Management Co., Ltd.
    Inventors: Yasuhiro FUNAHASHI, Kotaro KODAMA, Ryo DAIRIKI, Yukinori MINOSHIMA
  • Substituted n?-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
    Patent number: 10988487
    Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: April 27, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Abdelghani Achab, Purakkattle Biju, Timothy A. Cernak, Yongqi Deng, Xavier Fradera, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Derun Li, Guoqing Li, Qinglin Pu, Zhi-Cai Shi, Wensheng Yu, Hongjun Zhang
  • TRICYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20210115044
    Abstract: The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: April 22, 2019
    Publication date: April 22, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, James M. Apgar, Alan Whitehead, Yonglian Zhang, Zhiyong Hu, Valerie W. Shurtleff, John A. McCauley, Izzat T. Raheem
  • 5-(pyridin-3-yl)oxazole allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 10981902
    Abstract: The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: April 20, 2021
    Assignees: Merck Sharp & Dohme Corp., Merck MSD (R&D) China Co., LTD.
    Inventors: Jianming Bao, Timothy J. Henderson, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Meng Na, Michael T. Rudd, David M. Tellers, Ling Tong
  • 9-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
    Publication number: 20210107904
    Abstract: In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
    Type: Application
    Filed: November 26, 2019
    Publication date: April 15, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Matthew A. Larsen, Amjad Ali, Jared Cumming, Duane DeMong, Qiaolin Deng, Thomas H. Graham, Elisabeth Hennessy, Andrew J. Hoover, Ping Liu, Kun Liu, Umar Faruk Mansoor, Jianping Pan, Christopher W. Plummer, Aaron Sather, Uma Swaminathan, Huijun Wang, Yonglian Zhang
  • KDM5 inhibitors
    Patent number: 10975084
    Abstract: The present invention provides a compound of Formula (I) (represented as tautomers Ia and Ib) or the pharmaceutically acceptable salts thereof, which are KDM5 inhibitors.
    Type: Grant
    Filed: October 6, 2017
    Date of Patent: April 13, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Umar Faruk Mansoor, Christian Fischer, Phieng Siliphaivanh, Luis Torres, Hakan Gunaydin, David L. Sloman
  • Antidiabetic bicyclic compounds
    Patent number: 10968193
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: April 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Chen, Steven L. Colletti, Duane DeMong, Yan Guo, Michael Miller, Anilkumar Nair, Christopher W. Plummer, Dong Xiao, De-Yi Yang
  • Antidiabetic spirochroman compounds
    Patent number: 10968232
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: April 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Harry R. Chobanian, Shuwen He, Jinsong Hao, Barbara Pio, Yan Guo, Dong Xiao
  • Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels
    Patent number: 10968210
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: April 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet
  • DRUG DELIVERY SYSTEM FOR THE DELIVERY OF ANTIVIRAL AGENTS
    Publication number: 20210093555
    Abstract: This invention relates to novel implant drug delivery systems for long-acting delivery of antiviral drugs. These compositions are useful for the treatment or prevention of human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: April 5, 2018
    Publication date: April 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Stephanie Elizabeth Barrett, Marian E. Gindy, Li Li, Ryan S. Teller, Seth P. Forster
  • ANTIDIABETIC BICYCLIC COMPOUNDS
    Publication number: 20210094938
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia Formula (I).
    Type: Application
    Filed: November 12, 2018
    Publication date: April 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Duane DeMong, Kevin D. Dykstra, Zhiyong Hu, Michael Miller
  • RECOMBINANT EXPRESSION OF CHLAMYDIA MOMP ANTIGEN
    Publication number: 20210093703
    Abstract: The present invention relates to methods for the recombinant expression of chlamydia major outer membrane protein (MOMP) comprising transforming a population of E. coli host cells with an expression vector comprising a nucleic acid molecule that encodes chlamydia MOMP and encodes a leader sequence for targeting the MOMP to the outer membrane of the cell, wherein the nucleic acid molecule is operatively linked to a promoter. The method of the invention allows expression of MOMP in the outer membrane of the cell, which leads to protein folding that is more like native MOMP relative to a MOMP protein that is expressed intracellularly. Also provided by the invention are uses of the recombinant MOMP in pharmaceutical compositions and methods for the treatment and/or prophylaxis of chlamydia infection and/or the effects thereof.
    Type: Application
    Filed: June 8, 2020
    Publication date: April 1, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Lan Zhang, Zhiyun Wen, Craig T. Przysiecki, Puneet Khandelwal, Ping Qiu
  • N-aryl and N-heteroaryl piperidine derivatives as liver X receptor beta agonists, compositions, and their use
    Patent number: 10961215
    Abstract: In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
    Type: Grant
    Filed: October 9, 2017
    Date of Patent: March 30, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu
  • 4?-Substituted nucleoside reverse transcriptase inhibitors and preparations thereof
    Patent number: 10953029
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula (I) and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: March 23, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Vinay M. Girijavallabhan
  • Compounds inhibiting leucine-rich repeat kinase enzyme activity
    Patent number: 10954240
    Abstract: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R9, and A are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: March 23, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Kallol Basu, Duane DeMong, Sarah W. Li, Michael Miller, Jack D. Scott, Andrew W. Stamford